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Muscle Building And The Quest For Test

Posted in: Articles by ProSource, Supplement Articles, Tribulus Terrestris, ProSource: AndroTest
By Brian Batcheldor & the ProSource Research team | Feb 21, 2007

The Real Truth About Prohormones and the Natural T-boosting Alternatives

Muscle building has always been the primary objective for every bodybuilder, whether pro or amateur. With that, there can be no doubt that when it comes to the acquisition of superhuman strength and enviable virility, the male hormone testosterone is definitely the daddy! In fact, you would be hard pressed to find any individual who couldn't benefit from an extra helping of "Big T"--and that includes female athletes, too.

The use of certain prohormones (androstendione and 4-androstenediol) was once an option in achieving this goal. However, this was not the result of stimulation of natural (endogenous) testosterone production--merely a topping off and even the possible subsequent short-term suppression of these levels (negative feedback in the HPTA--Hypothalamus-Pituitary-Testicular Axis).

Now, apparently, this a moot point because of the prohormone controversy. Some feel that the crackdown on prohormones wasn't such a bad thing. After all, they brought nothing but adverse publicity to sports nutrition. At any rate, a host of nandrolone positives have fuelled draconian legislation that will limit the future rights of the world's supplement consumers.

But if prohormones stirred up unrest, then the latest "innovation" spawned by this legislation may even threaten the very existence of sports nutrition as an industry. With many a company having built its empire on prohormone sales over the past few years, the temptation to not let go was seemingly too great for some. Believing to have found a legal loophole, some companies are delivering a replacement that has essentially gone way beyond desperate. "Prohormones are back", we're being told. Well, don't believe it for a second, because what we're now being offered are far more sinister substitutions! Now, pregnane steroids, anabolic steroids modified by the addition of a methyl group, metabolites of known anabolic steroids, analogs of research anti-aromatase drugs and even of antiandrogens are being passed off as the "second coming" of prohormones. Some have chosen to throw up a smoke screen by labeling these as "proto-hormones." Others have merely opted for deceptive labeling, making it almost impossible to identify the active compound. What's more, the search is not over to find analogs of some of the most toxic anabolic steroids ever developed. Ironically, many of these compounds are being touted as pro-testosterone formulas, though nothing could be further from the truth. At best, one or two of these compounds may show promise as an anti-aromatase (e.g. 6,17-keto-etiocholeve-3-ol tetrahydropyranol), if further research was conducted, including toxicology studies. At worst, if you take these revised prohormone products, you will likely be taking a highly toxic steroid that could make you sick and shut down T production for a long time.

Let's get this straight. Metabolites of Oral Turinabol or stanazolol with a methyl group added (3,2-c]pyrazole-5alpha-etioallocholane-17beta-tetrahydropyranol) are not supplements, they're anabolic steroids with speculative potential. Ignore the hype, these could range from being completely weak to being more toxic than Halotestin! There's no research to base any real world results on. I have no problem with anabolic steroids, I have consulted on their use for years, written numerous articles and lectured on them all over the world. I would never actually advise anyone to initiate anabolic steroid use, but if given the choice between these new prohormone compounds and regular anabolic steroids, I know what I'd recommend. After all, with anabolics, like oxandrolone, Deca Durabolin and Sustenon, the research and years of anecdotal evidence is there so you can at least make an educated choice about their use.

Okay, so now we've established that these products are not even an option for those wishing to stimulate endogenous T levels, including those taking a break from anabolic steroids. We now need to head down the right pathway.

The Green Solution: Phytochemistry
Almost every culture has its own traditional product for the vital objective of natural testosterone elevation; from ayurvedic to Chinese medicine, from rainforest shaman to African witch doctor, they all have a special elixir guaranteed to put hair on your chest and lead in your pencil. But the aphrodisiac property of an indigenous herb (muira puama, catuaba, etc) may have nothing to do with testosterone. This could well be accounted for by an influence on serotonin or dopamine. It's also quite possible that these herbs could contain constituents that actually have a negative impact on testosterone or fertility; many herbs are known to have this effect. Conversely, some herbs that have known fertility enhancing properties have no impact on testosterone; Maca is an example here1.

The wealth of scientific expertise now employed within the herbal industry has been highly instrumental in its recent progression, particularly in the application of high-tech analytical methodology to the process of standardization. Where once the standard simply meant the ratio of raw material to the finished extract (e.g. a 10:1 extract), today it refers to a percentage of one or more phytochemical "fingerprints" derived from the original raw material. Breakthroughs in extraction technology, coupled with reliable analytical methodology, now mean that scientists are able to verify the properties of a particular herb, identify the active component responsible for the benefits and produce a finished extract with a consistent quantity of that component from batch to batch. Standardization is an absolute must now, but only if the correct form of analytical methodology has been used. It is also vital that the plant is standardized for the right component, as many herbs have numerous medicinal uses with different components responsible for each. The take-home message here is that if you're not using a pharmaceutical-grade standardized extract, then you're probably using inactive junk .

The exciting fact about these "fingerprint" components, be they saponins, alkaloids, tannins, phenols, flavonoids or whatever, is that their properties are often attributable to the ability to impact various biological systems in the human body. Several of these compounds have an established ability to exert hormone-like effects. For our objective, the system we need to influence is the endocrine system, or to be more specific, the HPT axis. There are several ways in which this can be achieved, including:
    1. Direct stimulation of the Leydig cells in the testes.
    2. Stimulation of the pituitary to produce more luteinizing hormone(LH).
    3. Reduction of estradiol levels, either through competitive receptor binding (anti-estrogens) or decreased production of the aromatase enzyme.
    4. Competitive binding of sex hormone-binding globulin (SHBG) to produce more biologically active ("free") testosterone.
    5. Increased production of the enzymesresponsible for the biosynthesis of testosterone.
Various indirect approaches could involve influencing the production of other hormones capable of impacting T levels. For example, reducing prolactin can increase testosterone, as can stimulating oxytocin or noradrenaline. The good news is that there are numerous herbs out there for which one or even several of the above properties have been identified.

The Contenders
Turning to the relevant scientific research, studies using human subjects are given priority, with those using multiple species being next, as there can be large differences in the results between different species2.

Stimulation of Leydig cell steroidogenesis occurs mainly through a cAMP mediated mechanism, which includes adenylate cyclase activation. Forskolin, isolated from the plant Coleus forskholii, is a popular ingredient in some thermogenic formulas and has a well-established ability to help stimulate adenylate cyclase and increase cyclic AMP. These abilities mean that forskolin is commonly used in scientific studies for the purpose of testosterone stimulation. Recently, a compound isolated from sage (Salvia sclarea), known as FSC, has demonstrated a similar activity profile to that of forskolin. FSC also aids in restoring the level of monoamines for presynaptic availability, giving this compound antidepressant properties. Several plant species are believed to have constituents that may stimulate LH release. One of these is Avena sativa, used for centuries for disabilities and as a nerve tonic. Japanese scientists have actually identified a substance in this plant that has potent LH-releasing activity, although it is structurally different from LH-RH present in the hypothalamus. Interestingly, garlic has also been shown to increase testosterone by enhancing LH production. The allyl-containing sulfides in garlic are known to stimulate the pituitary gland by increasing the concentration of noradrenaline. The anti-stress properties of garlic, which include reducing stress hormones, may also be partly responsible for this effect3,4.

Unfortunately, most plant constituents indicated to have anti-estrogenic properties have yet to get past the "in vitro" stage, while the few that have show poor oral bioavailability. The main classes of these phytoestrogens are isoflavanoids, phytoalexins and coumestans. One phytoalexin in particular, Resveratrol (3,5,4"-trihydroxystilbene), found in red wine and grapes, has demonstrated a powerful ability to impart the protective effects of estrogen on bone loss and cardiovascular disease in vivo5. This means that the estrogen antagonism that it has demonstrated in vitro could possibly be replicated after oral administration. Diindolyl methane, a dietary indole isolated from cruciferous vegetables, may be able to promote dramatic and beneficial changes in estrogen metabolism through various mechanisms. Backed by several in vivo studies, it has demonstrated competitive receptor binding and the ability to affect estrogen synthesis and its conversion to weaker metabolites. The real heavyweight contender amongst this section may well be calcium D-glucarate, a compound found in numerous fruits and vegetables. In studies, supplementation with this has been shown to affect estrogen by increasing levels of D-glucarolactone, thereby increasing the metabolism and excretion of estadiol6.

As I mentioned earlier, another way to potentially elevate testosterone is by decreasing prolactin. Specialized extracts of the herb Vitex agnus castus have effectively demonstrated this ability in vivo7, a group of components called agnusides have been identified as the active principles.

Herbs that may also exert a positive effect on T levels are those with established anti-stress properties. Of these, Rhodiola rosea and Morinda officinalis show real promise, as both of these have demonstrated an ability to support/increased testosterone under stressed conditions8,9. Epimedium, commonly used for the same purpose, has yet to get off the ground in my book, as it hasn't been shown to have any impact on testosterone and may actually elevate cortisol10.

The Heavyweight
Although Tribulus terrestris has enjoyed a reputation as a major player in the testosterone stakes, it has never really achieved its full muscle building potential. That is, until recently. One big breakthrough came when it was finally determined through years of intensive scientific investigation that the true and most potent active compound found in tribulus is a steroidal saponin called protodioscin. Protodioscin has been shown to significantly enhance the body's production of luteinizing hormone, consequently raising testosterone levels at a remarkable rate. It has been further shown to also help stimulate protein synthesis, which is a major factor for lean mass growth. Bulgarian grown tribulus is well known to contain the highest markers of protodioscin content due to its rich soil and growing conditions. Although some manufacturers offer products that do contain some tribulus and small amounts of protodioscin, I have found only one company that delivers a true, body-changing amount of protodioscin. The reason, I have learned, for this alarming difference in potency, is due to a multiple extraction process that goes far beyond what other companies are doing. When you start with the best Bulgarian trib available and subject it to state-of-the-art processing, the numbers speak for themselves. The ProSource research team lay claim to accomplishing something that no other company has even come close to matching. Their AndroTest product is standardized to contain 40 to 48% protodioscin, which is an unheard of potency, until now. Based on this potency, it seems clear that what we have here is an authentic natural substitute for the aforementioned prohormones.

The Other Real Deal
By the time this goes to print, still few of you will have heard of Tongkat Ali, a traditional Malaysian aphrodisiac prepared from the herb Eurycoma longifolia. But trust me, this obscure Asian plant looks to be the most exciting and effective breakthrough in the quest for optimal testosterone enhancement!

Although it may have many uses in various Asian cultures, the most common use for this herb is as a "bestower of superhuman virility." Around three years ago, I "hacked" into some serious research being conducted by the East Asian medical world, where this herb was being considered as potential treatment for infertility and impotence. Since then, I've been working with Eurycoma non-stop and can tell you that other than protodioscin there's nothing else out there that even comes close to this herb as a serious T booster. It's rock solid reputation is heavily backed up by numerous unrelated, unbiased scientific studies--both in vitro and in vivo, in multiple animal species and in humans. These studies include:
  • Effects on energy production systems.
  • Sexual behaviour and mating studies.
  • Hormone studies.
  • Studies on anabolic properties.
  • IVF studies.
  • Sperm characteristic studies.
  • Toxicity studies.
What exactly have these studies shown? Many things, but just to whet your appetite, take a look at its established impact on the testosterone levels of animals:

Animal % increased
Mice 479%
Rat 380%
Rabbit 320%

As if this isn't impressive enough, in human testicular tissue the same extract yielded a 440% increase11! Taking a look at what this translates to in the real world, human infertility studies have also revealed a suitably impressive testosterone response. So far, its potent pro-testosterone properties have been attributed to three different mechanisms, they are:
    1. Increased substrate enzymes for the biosynthesis of testosterone.
    2. Increased cAMP.
    3. Decreased SHBG.
In another in vivo study, this time using trained subjects, specific anabolic properties were identified12. But to fully exploit Eurycoma's awesome potential, you need to first overcome an inherent problem. Basically, the presence of bitter components, known as quassinoids, have given Eurycoma its other scientifically proven activities (e.g. anti-malarial, anti-tumour and anti-inflammatory). However, recent advances in manufacturing have been implemented to eliminate this problem with the correct extraction process, thereby developing a pharmaceutical grade extract. The finer details of exciting new research coming out of the U.S., Korea and Japan will likely soon become available. But for the time being, it seems that Eurycoma is set to take the bodybuilding world by storm!

On the horizon
The latest addition to the herbal pro-testosterone market is an extract of fenugreek standardized for what the vendors have chosen to call Fenuside. There are ongoing studies occurring with this material, but those currently available mostly relate to the sexual performance of rats when compared with sildenafil use. Although many companies have been sold on this story, at best, I think it may hold a little promise.

It is the hope of our company that this article has helped shed some light on the growing concerns relegated to the "new" prohormones out there, and the growing acceptance of several truly powerful T-boosting herbals. Again, standardized protodiscin content is the most critical factor to be looking for when choosing a next generation T-booster. That, and standardized Tongkat Ali, offer the most beneficial results. As mentioned earlier, the product AndroTest actually contains the highest amounts of both of these, and other saponins, making this synergistic dynamo a scientific breakthrough unprecedented in the natural T-boosting realm. This impressive new technology is bound to create an enormous buzz throughout the bodybuilding community as one individual after another experiences the kind of results once only relegated to the synthetics of the past.

(1). Gonzales GF et al. Effect of Lepidium meyenii (Maca), a root with aphrodisiac and fertility-enhancing properties, on serum reproductive hormone levels in adult healthy men. J Endocrinol 2003 Jan;176(1):163-8.
(2). Chambers KC et al. Apomorphine, deprenyl, and yohimbine fail to increase sexual behavior in rhesus males. Behav Neurosci 1989 Aug;103(4):816-23
(3). Kasuga S et al. Pharmacologic activities of aged garlic extract in comparison with other garlic preparations. J Nutr 2001 Mar;131(3s):1080S-4S.
(4). Fukushima M et al. Extraction and purification of a substance with luteinizing hormone releasing activity from the leaves of Avena sativa. Tohoku J Exp Med 1976 Jun;119(2):115-22.
(5). Resveratrol attenuates ovariectomy-induced hypertension and bone loss in stroke-prone spontaneously hypertensive rats. J Nutr Sci Vitam inol (Tokyo) 2000 Apr;46(2):78-83.
(6). Walaszek Z et al. Reduced levels of D-Glucaric acid in mammary tumor-bearing hosts and the effect of its supplementation during estrogen replacement and tamoxifin therapy. Proc. Am. Assoc. Cancer Res. 37: 183.
(7). Gorkow C et al. Effectiveness of Vitex agnus-castus preparations. Wien Med Wochenschr 2002;152(15-16):364-72
(8). Lishmanov I et al. Plasma beta-endorphin and stress hormones in stress and adaptation. Biull Eksp Biol Med 1987 Apr;103(4):422-4.
(9). Li YF et al. Antistress effect of oligosaccharides extracted from Morinda officinalis in mice and rats. Acta Pharmacol Sin 2001 Dec;22(12):1084-8.
(10). Kuang AK et al. Effects of yang-restoring herb medicines on the levels of plasma corticosterone, testosterone and triiodothyronine. Zhong Xi Yi Jie He Za Zhi 1989 Dec;9(12):737-8, 710.
(11). Saad J M et al. The effect of Eurycoma longifolia on rat and human testicular steroidogenesis. Dept of Biochem and surgery, Faculty of med, Univ of Malaysia.
(12). Tambi I. Anabolic effect of Eurycoma longifolia jack, 2002. Univ of Malaysia.


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